Assay Detail
Binding
CHEMBL3267681
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]radioligand from human orexin-1 receptor expressed in CHO cells after 3 hrs by scintillation counting analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 9.13 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3260826 | — | — | 1 | 9.70 |
| CHEMBL3260828 | — | — | 1 | 9.52 |
| CHEMBL3260835 | — | — | 1 | 9.52 |
| CHEMBL3260836 | — | — | 1 | 9.52 |
| CHEMBL3260833 | — | — | 1 | 9.40 |
| CHEMBL3260827 | — | — | 1 | 9.30 |
| CHEMBL3260831 | — | — | 1 | 9.30 |
| CHEMBL1083659 | SUVOREXANT | 4.0 | 1 | 9.22 |
| CHEMBL3260834 | — | — | 1 | 9.15 |
| CHEMBL3260824 | — | — | 1 | 9.10 |
| CHEMBL3260832 | — | — | 1 | 9.05 |
| CHEMBL3260829 | — | — | 1 | 8.74 |
| CHEMBL3260830 | — | — | 1 | 8.74 |
| CHEMBL1083358 | — | — | 1 | 8.74 |
| CHEMBL3260823 | — | — | 1 | 8.70 |
| CHEMBL3260825 | — | — | 1 | 8.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3260826 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3260828 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3260835 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3260836 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3260833 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL3260827 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL3260831 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL1083659 | SUVOREXANT | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL3260834 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3260824 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL3260832 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL3260829 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3260830 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL1083358 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL3260823 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3260825 | — | Ki | = | 4.5 | nM | 8.35 |